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Optimized flurbiprofen sustained-release matrix pellets prepared by extrusion/spheronization
Journal of Drug Delivery Science and Technology ( IF 4.5 ) Pub Date : 2020-07-16 , DOI: 10.1016/j.jddst.2020.101902
Doaa Hasan Alshora , Mohamed Abbas Ibrahim , Essam Ezzeldin , Muzaffar Iqbal

Flurbiprofen (FBP) is an ibuprofen derivative with less gastric side effects and short biological half-life (4.7–5.7 h). The study aimed to formulate FBP as a sustained-release pellets by extrusion/spheronization to overcome its short half-life and to decrease dose frequency. The wet mass of the pellets containing Avicel® and a polymeric matrix polymer was determined by measuring the mean line torque. The impacts of different types and concentrations of matrix-forming units (HPMC, Carbopol, and PVP) (independent variables) on pellet size, mean line torque, and dissolution rate after 8 h were assessed using the Box-Behnken design. The results showed that the formulation containing higher concentrations of HPMC and Carbopol, such as F14, had high mean line torque value. This high mean line torque was responsible for the increased pellet size (>1100 μm) and decreased release rate (68 ± 2.8%) after 8 h of F14, compared with those of F5, which did not contain HPMC or Carbopol and had the lowest mean line torque, smallest pellet size (875.9 ± 27.5 μm), and highest dissolution rate after 8 h (100 ± 5.9%). In conclusion, sustained-release pellet formulation of FBP was able to sustain the release of FBP for up to 8 h.



中文翻译:

通过挤出/滚圆法制备的优化的氟比洛芬缓释基质药丸

氟比洛芬(FBP)是一种布洛芬衍生物,具有较少的胃部副作用和较短的生物学半衰期(4.7-5.7小时)。该研究旨在通过挤出/滚圆法将FBP制成缓释微丸,以克服其短的半衰期并降低给药频率。通过测量平均线扭矩确定含有和聚合物基聚合物的粒料的湿质量。使用Box-Behnken设计评估了8小时后,不同类型和浓度的基质形成单元(HPMC,Carbopol和PVP)(独立变量)对颗粒大小,平均线扭矩和溶出度的影响。结果表明,含有较高浓度的HPMC和Carbopol的配方(例如F14)具有较高的平均线扭矩值。较高的平均线扭矩导致颗粒尺寸增大(> 与不含HPMC或Carbopol且平均线扭矩最低,粒料尺寸最小(875.9±27.5μm)的F5相比,F14 8 h后的1100μm释放速率降低(68±2.8%), 8小时后溶出率最高(100±5.9%)。总之,FBP的缓释微丸制剂能够维持FBP的释放长达8小时。

更新日期:2020-07-16
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